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Abstract：
Flavonoids are an abundant class of naturally occurring compounds with broad biological activities, but their limited abundance in nature restricts their use in medicines and food additives. Here we present the synthesis and determination of the antibacterial and antioxidant activities of twenty-two structurally related flavonoids (five of which are new) by scientifically validated methods. Flavanones (FV1-FV11) had low inhibitory activity against the bacterial growth of MRSA 97-7. However, FV2 (C5,7,3\',4\' = OH) and FV6 (C5,7 = OH; C4\' = SCH3) had excellent bacterial growth inhibitory activity against Gram-negative E. coli (MIC = 25 µg/mL for both), while Chloramphenicol (MIC = 25 µg/mL) and FV1 (C5,7,3\' = OCH3; 4\' = OH) showed inhibitory activity against Gram-positive L. monocytogenes (MIC = 25 µg/mL). From the flavone series (FO1-FO11), FO2 (C5,7,3\',4\' = OH), FO3 (C5,7,4\' = OH; 3\' = OCH3), and FO5 (C5,7,4\' = OH) showed good inhibitory activity against Gram-positive MRSA 97-7 (MIC = 50, 12, and 50 µg/mL, respectively), with FO3 being more active than the positive control Vancomycin (MIC = 25 µg/mL). FO10 (C5,7= OH; 4\' = OCH3) showed high inhibitory activity against E. coli and L. monocytogenes (MIC = 25 and 15 µg/mL, respectively). These data add significantly to our knowledge of the structural requirements to combat these human pathogens. The positions and number of hydroxyl groups were key to the antibacterial and antioxidant activities.
摘要：
类黄酮是一类丰富的天然化合物，具有广泛的生物活性，但是它们在自然界中的有限丰度限制了它们在药物和食品添加剂中的使用。在这里，我们介绍了通过科学验证的方法合成和测定22种结构相关的类黄酮（其中5种是新的）的抗菌和抗氧化活性。黄酮类(FV1-FV11)对MRSA97-7的细菌生长具有低抑制活性。然而,FV2（C5,7,3\'，4\'=OH）和FV6（C5,7=OH；C4\'=SCH3）对革兰氏阴性大肠杆菌（MIC=25µg/mL）具有出色的细菌生长抑制活性，而氯霉素（MIC=25µg/mL）和FV1（C5,7,3\'=OCH3；4\'=OH）对革兰氏阳性单核细胞增生李斯特菌（MIC=25µg/mL）具有抑制活性。从黄酮系列（FO1-FO11），FO2（C5,7,3\'，4\'=OH)，FO3(C5,7,4\'=OH；3\'=OCH3)，和FO5（C5,7,4\'=OH）对革兰氏阳性MRSA97-7（MIC=50、12和50µg/mL，分别)，FO3比阳性对照万古霉素更具活性（MIC=25µg/mL）。FO10（C5,7=OH；4'=OCH3）对大肠杆菌和单核细胞增生李斯特菌显示出高抑制活性（MIC=25和15µg/mL，分别)。这些数据大大增加了我们对对抗这些人类病原体的结构要求的认识。羟基的位置和数量是抗菌和抗氧化活性的关键。
